One-Pot Synthesis of 2-Amino-indole-3-carboxamide and Analogous

An efficient one-pot, two-step solution-phase synthetic method was developed to synthesize twenty-three 2-amino-indole-3-carboxamides (3) from 2-halonitrobenzene (1) or heterocyclic analogous and cyanoacetamides (2). In this sequence, first, intermediate 2-cyano-2-(2-nitrophenyl)acetamide (4) was generated under basic condition via S_NAr reaction; after direct addition of hydrochloric acid solution, FeCl₃, and Zn powder, indole 3 was generated via reduction/cyclization process.